Adverse Drug Reaction Classification System

Pharmaceutical Information
Drug Name Tofacitinib
Drug ID BADD_D02236
Description Tofacitinib is an inhibitor of Janus kinases, a group of intracellular enzymes involved in signalling pathways that affect hematopoiesis and immune cell function. It is approved by the FDA for treatment of moderate to severe rheumatoid arthritis that responds inadequately to methotrexate or in those who are intolerant to methotrexate. Besides rheumatoid arthritis, tofacitinib has also been studied in clinical trials for the prevention of organ transplant rejection, and is currently under investigation for the treatment of psoriasis. Known adverse effects include nausea and headache as well as more serious immunologic and hematological adverse effects. Tofacitinib is marketed under the brand name Xeljanz by Pfizer.
Indications and Usage For the treatment of moderate to severe rheumatoid arthritis which is resistant or intolerant to methotrexate therapy. It may also be used as an adjunct to methotrexate therapy, or other non-biologic disease-modifying antirheumatic drugs (DMARDS), when methotrexate alone is not sufficient. Tofacitinib has also been investigated as a preventative therapy for kidney transplant rejections, and as a treatment for psoriasis, ulcerative colitis, and ankylosing spondylitis. It is not to be initiated in patients with a history of chronic or recurrent infections, or in the presence of active infection, even if localized, due to reports of serious and sometimes fatal infections (commonly pneumonia, herpes zoster and urinary tract infections). Use of tofacitinib is also discouraged in those who have been, or are likely to be, exposed to TB. An increased likelihood of exposure may be encountered by traveling to certain areas. In addition, tofacitinib is not to be used in patients with severe hepatic impairment, or low hemoglobin (less than 9g/dL). Cautioned is advised when using tofacitinib in patients at risk of gastrointestinal perforation, and in the elderly who are more susceptible to infection.
Marketing Status approved; investigational
ATC Code L04AA29
DrugBank ID DB08895
KEGG ID D09970
MeSH ID C479163
PubChem ID 9926791
TTD Drug ID D0EG1I
NDC Product Code 0069-1002; 63539-012; 0069-0502; 42816-0501; 63539-501; 0069-0501; 0069-1001; 0069-1029; 63539-016; 63539-502; 71796-050
UNII 87LA6FU830
Synonyms tofacitinib | tasocitinib | tofacitinib citrate | Xeljanz | CP 690,550 | CP690550 | CP-690550 | CP 690550 | CP-690,550
Chemical Information
Molecular Formula C16H20N6O
CAS Registry Number 477600-75-2
SMILES CC1CCN(CC1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N
Chemical Structure
ADRs Induced by Drug
*The priority for ADR severity classification is based on FAERS assessment, followed by the most severe level in CTCAE rating. If neither is available, it will be displayed as 'Not available'.
**The 'Not Available' level is hidden by default and can be restored by clicking on the legend twice..
ADR Term ADReCS ID ADR Frequency (FAERS) ADR Severity Grade (FAERS) ADR Severity Grade (CTCAE)
Neoplasm recurrence16.16.02.0040.001013%Not Available
Obstruction08.01.03.0230.000651%Not Available
Pancreatic neoplasm16.13.11.005; 07.21.09.0040.000241%Not Available
Food intolerance14.02.01.0050.000820%Not Available
Hepatobiliary disease09.01.08.003--Not Available
Immunosuppression10.03.02.0010.005304%Not Available
Hyperlipidaemia14.08.03.0010.015431%
Knee deformity15.10.03.0020.001881%Not Available
Pigmentation disorder23.05.03.001--Not Available
Renal mass20.01.02.0070.000530%Not Available
Nasal disorder22.04.03.0040.003810%Not Available
Renal impairment20.01.03.010--Not Available
Sinus disorder22.04.06.0020.049091%
Nail ridging23.02.05.0200.001350%
Joint hyperextension15.01.08.003; 12.04.03.0040.000940%Not Available
Poor quality sleep19.02.05.005; 17.15.04.0020.016950%Not Available
Middle ear effusion04.05.03.0010.002170%Not Available
Arterial occlusive disease24.04.02.0210.001254%Not Available
Haemorrhagic diathesis01.01.03.003; 24.07.01.0200.001133%Not Available
Increased upper airway secretion22.12.03.0070.001230%Not Available
Effusion08.01.03.0520.002291%Not Available
Postural orthostatic tachycardia syndrome17.05.01.019; 02.03.02.0200.000362%Not Available
Bowel movement irregularity07.02.03.0030.022231%Not Available
Erosive oesophagitis07.04.05.0040.000362%Not Available
Solar lentigo23.05.01.0130.000820%Not Available
Gastrointestinal inflammation07.08.03.0070.001953%Not Available
Skin haemorrhage24.07.01.103; 23.06.07.001--Not Available
Muscle swelling15.05.03.0150.001881%Not Available
Oral mucosal exfoliation07.05.05.0110.000241%Not Available
Breakthrough pain16.32.03.016; 08.01.08.0260.006920%Not Available
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